JPH0383912A - Composition for oral cavity - Google Patents

Abstract

PURPOSE:To provide a stable oral cavity composition having an excellent protecting activity, exhibiting excellent depressing and improving activities against gingivitis and other diseases and having excellent taste and freshness on the employment thereof by containing a specific compound as an active ingredient. CONSTITUTION:A composition for oral cavities contains 3-[p-(trans-4- aminomethylcyclohexylcarbonyl)phenyl]propionic acid (compound A) or a salt thereof as an active ingredient. The salt of the compound A includes inorganic or organic acid salts such as hydrochloric acid salt, sulfuric acid salt, fumaric acid salt and maleic acid salt and alkali (ne earth) metal salts such as Na salt, K salt, Ca salt and Mg salt and is contained in a weight ratio of usually 0.01-0.1% in the composition. The composition may be coated on a onset portion of skin in a suitable amount several times a day and the skin may be massaged or blushed. The composition are used for tooth pastes, liquid dentifrices, pastas, etc.

Description

Detailed Description of the Invention Industrial Field of Application The present invention provides 3-[p-(trans-4-aminomethylcyclohexylcarbonyl)phenyl]propionic acid (
The present invention relates to an oral composition containing Compound A) or a salt thereof.

<Conventional technology> In general, in the field of dentistry, periodontal disease, including internal inflammation and alveolar pyorrhea, is said to be one of the three major diseases along with dental caries, and the prevalence of these diseases is currently extremely high. . Therefore, it is extremely important for dental prevention to perform daily dental cleanings and gum surgery.

As a means of achieving this, it is an extremely effective and rational means to use a dentifrice or paste agent that is effective in removing dental impurities, suppressing the occurrence of gingival inflammation, and cleaning the oral cavity. However, conventional dentifrices and paste preparations all have their advantages and disadvantages, and few are fully satisfactory. , things that are destroyed by heat, a′
Rui often has a bitter or astringent taste or impairs the cooling sensation, making it impractical, and there are also problems with coloring, cost, solubility, resources, and even safety.

<Problems Solved by the Invention> As a result of intensive studies to solve the above-mentioned problems, the present inventors found that an oral composition containing Compound A or a salt thereof satisfies the purpose. Completed the invention.

<Configuration of the Invention> The present invention relates to an oral composition containing Compound A or a salt thereof.

Examples of the oral composition according to the present invention include toothpaste agents, liquid dentifrices, paste agents, and the like.

Examples of salts of compound A include hydrochloric acid, sulfuric acid, and fumaric acid.

Acid addition salts of inorganic or organic acids such as maleic acid.

Also, alkali metal salts or alkaline earth metal salts such as sodium salts, potassium salts, calcium salts, and magnesium salts of carboxyl groups can be mentioned.

The above-mentioned oral composition can be manufactured by appropriately using known formulation techniques, and the content of Compound A or its salt in the composition may usually be about 0.01 to 01k (weight ratio). .

The oral composition of the present invention may be applied in an appropriate amount to the affected area for several days, followed by massage or brushing.

Compound A and its salts had no problems in terms of safety, and their acute toxicity value (LDio) was 1600 mg/kg or more in mice (Ura) when administered orally.

<Effects of the Invention> The oral composition of the present invention has an excellent protective effect on periodontal tissue, and has an excellent suppressive and ameliorating effect on periodontal disease and its symptoms. This was confirmed by a test using a model (see JP-A-60-146815). In addition, in the oral composition of the present invention, the active ingredient Compound A and its salt were able to exist extremely stably. Furthermore.

When the oral composition of the present invention is used.

It has excellent taste and refreshing feeling.

Therefore, the present invention is excellent as an oral composition for periodontal disease.

The present invention will be further explained below with reference to Examples and Test Examples, but the present invention is not limited thereto.

Example 1 Compound A hydrochloride 50 mg Calcium hydrogen phosphate 508 Glycerin 30 g Sodium carboxymethyl cellulose 0.5 g Sodium lacryl sulfate tg Sodium saccharin
0.1 g purified water dosage meter too g A toothpaste was prepared according to the above recipe.

Example 2 Commercially available toothpaste (White and White: trade name,
(manufactured by Lion Corporation) 99.9g of compound A hydrochloride 0.1
g and mix well to make a total amount of 100 g of polishing agent.

Example 3 Commercially available pasta preparation (Parapunto Ace: trade name, manufactured by Lion Corporation) 99.5g e 0.5g of hydrochloride of compound A was added and mixed well to prepare a total amount of 100g of pasta preparation.

Test Example 1 25 μg of thrombin was added to ZOO μl of a suspension of compound A hydrochloride and Tris-buffered saline in an ice bath to prepare a test solution. Streptokinase 25 was added to this test solution.
µg and 100 µg of xifibrinogen were added, and the fibrin dissolution time was measured at 37°C. Time until fibrin dissolves (hemolysis)
) means that the longer the bleeding prevention effect is, the higher the bleeding prevention effect. The results are shown in Table 1 below.

Table 1 Inhibition rate (zero) Specimen 1ysls ime As is clear from the above, Compound A showed an excellent bleeding prevention effect. Since bleeding is a typical symptom of periodontal disease, it was confirmed that Compound A has an excellent suppressive effect on the symptoms of periodontal disease.

Test Example 2 The toothpastes and paste preparations of Examples 1 to 3 were heated to room temperature or 40°C.
The residual rate of Compound A in the preparation was examined by the method shown below.

100 ml of purified water was added to 4 g of the specimen, and the mixture was suspended by shaking for about 10 minutes. After centrifuging a portion of this liquid, the supernatant liquid was filtered through a membrane filter with a pore size of 0.45 μm to obtain a sample solution. Separately, 20 mg of Compound A was dissolved in purified water to give 100011. Purified water was added to 10 ml of this solution to make 50a+1, which was used as a standard solution.

10 μl each of the sample solution and standard solution were analyzed by liquid chromatography under the following measurement conditions.

(Measurement conditions) Detector: Ultraviolet absorption photometer Wavelength 256t+a+h ?
Mu: :2 Sumosil 5 (is 4.eφX 150m
m Mobile phase: O,05M phosphate buffer (p)I 2.5
): Water: Methanol concentration 12:48:40 Flow rate: 0.8ml/sin.

Temperature = 40° C. The residual rate of Compound A at the start of storage was set to 100 zero. The results are shown in Table 2.

Table 2 As is clear from the above table, it was confirmed that the oral composition of the present invention has excellent stability of its active ingredients.

Claims (1)

[Claims] Oral composition containing 3-[p-(trans-4-aminomethylcyclohexylcarbonyl)phenyl]propionic acid or a salt thereof